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WO1992010504A3 - Phosphonic acid derivatives useful as antiinflammatory agents - Google Patents

Phosphonic acid derivatives useful as antiinflammatory agents Download PDF

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Publication number
WO1992010504A3
WO1992010504A3 PCT/US1991/008817 US9108817W WO9210504A3 WO 1992010504 A3 WO1992010504 A3 WO 1992010504A3 US 9108817 W US9108817 W US 9108817W WO 9210504 A3 WO9210504 A3 WO 9210504A3
Authority
WO
WIPO (PCT)
Prior art keywords
bisphosphonic acid
methylene
bis
tetramethyl ester
acid tetramethyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US1991/008817
Other languages
French (fr)
Other versions
WO1992010504A2 (en
Inventor
Roy Allen Johnson
Herman Walden Smith
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pharmacia and Upjohn Co
Original Assignee
Upjohn Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Upjohn Co filed Critical Upjohn Co
Priority to JP4501562A priority Critical patent/JPH06503329A/en
Priority to DE69108739T priority patent/DE69108739T2/en
Priority to EP92901352A priority patent/EP0561948B1/en
Publication of WO1992010504A2 publication Critical patent/WO1992010504A2/en
Publication of WO1992010504A3 publication Critical patent/WO1992010504A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/650952—Six-membered rings having the nitrogen atoms in the positions 1 and 4
    • C07F9/650994—Six-membered rings having the nitrogen atoms in the positions 1 and 4 condensed with carbocyclic rings or carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839—Polyphosphonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4025—Esters of poly(thio)phosphonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • C07F9/657181—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and, at least, one ring oxygen atom being part of a (thio)phosphonic acid derivative

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Filtration Of Liquid (AREA)

Abstract

Novel acids, esters, and salts of phenyl, naphtyl, quinoxalinyl, and biphenyl bisphosphonic acids and 1,2-oxaphosphepins are described. These compounds are useful as antiinflammatory and anti-arthritic agents. Also described are known compounds of the phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonate classes which are also useful as antiinflammatory and anti-arthritic agents. Representative compounds include [1,2-phenyldiyl]-bis(methylene)bisphosphonic acid tetramethyl ester, [2,3-quinoxalindiyl]bis(methylene)bisphosphonic acid tetramethyl ester, [[3-(propyl)-4-(methoxy)-1,8-naphthalenediyl]bis-(methylene)]bisphosphonic acid tetramethyl ester, [2,6-naphthalenediylbis(methylene)bisphosphonic acid tetraethyl ester, and [2,2'-biphenylenebis(methyl)]bisphosphonic acid tetramethyl ester. Representative oxaphosphepins include the preferred 3,4-dihydro-3-methoxy-7-(phenylmethoxy)-1H-naphth[1,8de][1,2]oxaphosphepin-3-oxide.
PCT/US1991/008817 1990-12-07 1991-12-03 Phosphonic acid derivatives useful as antiinflammatory agents Ceased WO1992010504A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP4501562A JPH06503329A (en) 1990-12-07 1991-12-03 Phosphonic acid derivatives useful as anti-inflammatory agents
DE69108739T DE69108739T2 (en) 1990-12-07 1991-12-03 PHOSPHONIC ACID DERIVATIVES AS AN ANTI-FLAMMING AGENTS.
EP92901352A EP0561948B1 (en) 1990-12-07 1991-12-03 Phosphonic acid derivatives useful as antiinflammatory agents

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US62411990A 1990-12-07 1990-12-07
US924,119 1990-12-07

Publications (2)

Publication Number Publication Date
WO1992010504A2 WO1992010504A2 (en) 1992-06-25
WO1992010504A3 true WO1992010504A3 (en) 1992-09-17

Family

ID=24500731

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1991/008817 Ceased WO1992010504A2 (en) 1990-12-07 1991-12-03 Phosphonic acid derivatives useful as antiinflammatory agents

Country Status (8)

Country Link
US (2) US5298498A (en)
EP (2) EP0561948B1 (en)
JP (1) JPH06503329A (en)
AU (1) AU9097791A (en)
CA (1) CA2094123A1 (en)
DE (1) DE69108739T2 (en)
DK (1) DK0561948T3 (en)
WO (1) WO1992010504A2 (en)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992010504A2 (en) * 1990-12-07 1992-06-25 The Upjohn Company Phosphonic acid derivatives useful as antiinflammatory agents
JPH08501794A (en) * 1992-09-23 1996-02-27 ジ・アップジョン・カンパニー Arylmethylphosphonates and phosphonic acids useful as anti-inflammatory agents
JP3951367B2 (en) * 1996-11-28 2007-08-01 住友化学株式会社 Stabilizer for thermoplastic resin containing pentavalent phosphorus compound as active ingredient, its production method and its use
GB2326369B (en) * 1997-06-20 2001-06-27 Aea Technology Plc Double lid system
US6096730A (en) * 1997-07-24 2000-08-01 University Of Kentucky Research Foundation Phosphonated agents and their antiangiogenic and antitumorigenic use
US5932563A (en) * 1998-10-23 1999-08-03 Ohio State Research Foundation Methods for treating spinal cord injury
US6627215B1 (en) * 1998-12-30 2003-09-30 Oligos Etc. Inc. Devices for improved wound management
US7868162B2 (en) * 1998-12-30 2011-01-11 Lakewood-Amedex, Inc. Antimicrobial and antiviral compounds and methods for their use
US20020032164A1 (en) * 1998-12-30 2002-03-14 Dale Roderic M. K. Antimicrobial compounds and methods for their use
ES2246234T3 (en) 1999-05-04 2006-02-16 Strakan International Limited ANDROGEN GLYCOSIDS AND ANDROGENIC ACTIVITY OF THE SAME.
JP4164718B2 (en) * 1999-10-06 2008-10-15 ソニー株式会社 Bis (aminostyryl) naphthalene compound and synthetic intermediate thereof, production method thereof, and organic electroluminescent device
EP1554572B1 (en) 2001-07-25 2009-10-14 Raptor Pharmaceutical Inc. Compositions and methods for modulating blood-brain barrier transport
CN102379684B (en) 2005-04-28 2014-11-19 普罗透斯数字保健公司 Pharma-informatics system
WO2007076462A2 (en) * 2005-12-22 2007-07-05 Oakwood Laboratories, Llc Sublimable sustained release delivery system and method of making same
US8795627B2 (en) 2007-03-21 2014-08-05 Raptor Pharmaceuticals Inc. Treatment of liver disorders by administration of RAP conjugates
ES2720080T3 (en) 2007-11-14 2019-07-17 Fresenius Kabi Austria Gmbh Continuous procedure for the preparation of crystalline lactulose
CN102316902B (en) 2009-02-20 2014-09-24 to-BBB控股股份有限公司 Glutathione-based drug delivery system
IL295075A (en) 2009-05-06 2022-09-01 Laboratory Skin Care Inc Preparations for administration through the skin that include complexes of an active substance with calcium phosphate and methods of using them
US20120077778A1 (en) 2010-09-29 2012-03-29 Andrea Bourdelais Ladder-Frame Polyether Conjugates

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1124949B (en) * 1960-03-04 1962-03-08 Basf Ag Process for the preparation of compounds of the 1,2-bis (vinyl) benzene series
EP0085321A2 (en) * 1982-01-27 1983-08-10 Schering Aktiengesellschaft Diphosphonic acid derivatives and pharmaceutical preparations containing them
EP0149802A2 (en) * 1983-12-21 1985-07-31 Hoechst Aktiengesellschaft 2,3-Bis(arylethényl)quinoxalines, process for their preparation and their use as photoconducting compounds

Family Cites Families (14)

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FR1541025A (en) * 1967-08-01 1968-10-04 Prec Mecanique Labinal Improvements to filters, in particular of the replaceable type, and more especially of plastic
CH558424A (en) * 1968-01-15 1975-01-31 Ciba Geigy Ag Styryl-naphthalene derivatives as optical brighteners
US3683080A (en) * 1970-08-28 1972-08-08 Procter & Gamble Compositions for inhibiting anomalous deposition and mobilization of calcium phosphate in animal tissue
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JPS57209424A (en) * 1981-06-17 1982-12-22 Nissan Motor Co Ltd Holder for fuel strainer
FR2531088B1 (en) * 1982-07-29 1987-08-28 Sanofi Sa ANTI-INFLAMMATORY PRODUCTS DERIVED FROM METHYLENEDIPHOSPHONIC ACID AND THEIR PREPARATION METHOD
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Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1124949B (en) * 1960-03-04 1962-03-08 Basf Ag Process for the preparation of compounds of the 1,2-bis (vinyl) benzene series
EP0085321A2 (en) * 1982-01-27 1983-08-10 Schering Aktiengesellschaft Diphosphonic acid derivatives and pharmaceutical preparations containing them
EP0149802A2 (en) * 1983-12-21 1985-07-31 Hoechst Aktiengesellschaft 2,3-Bis(arylethényl)quinoxalines, process for their preparation and their use as photoconducting compounds

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
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Chemical Abstracts, vol. 90, no. 13, 26 March 1979, (Columbus, Ohio, US), L. MAIER et al.: "Organic phosphorus compounds. 70. Preparation and properties of new phosphorus containing chelating agents for calcium and magnesium ions", see page 605, abstract no. 104063x, & PHOSPHORUS SULFUR 1978, 5(1), 45-51, see the abstract *
Journal of the American Chemical Society, vol. 93, no. 3, 10 February 1971, J. MEINWALD et al.: "Photochemical reactions of 1,8-divinylnaphthalene and 1,8-distyrylnaphthalene", pages 725-731, see page 726, compound 13; page 729, column 2, middle *

Also Published As

Publication number Publication date
EP0561948A1 (en) 1993-09-29
DE69108739D1 (en) 1995-05-11
EP0561948B1 (en) 1995-04-05
DE69108739T2 (en) 1995-09-14
CA2094123A1 (en) 1992-06-08
JPH06503329A (en) 1994-04-14
WO1992010504A2 (en) 1992-06-25
US5360797A (en) 1994-11-01
US5298498A (en) 1994-03-29
EP0622373A1 (en) 1994-11-02
DK0561948T3 (en) 1995-08-21
AU9097791A (en) 1992-07-08

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